411235-57-9Relevant articles and documents
2-amino-5-heteroaryl substituted pyrazine derivative and application thereof
-
Paragraph 0077-0078; 0080, (2021/05/29)
The invention provides a 2-amino-5-heteroaryl substituted pyrazine derivative with a chemical structure as shown in a formula 1, a pharmaceutical preparation containing the 2-amino-5-heteroaryl substituted pyrazine derivative, and application of the 2-amino-5-heteroaryl substituted pyrazine derivative in drugs for treating or preventing malaria. Compared with the prior art, the compound has the effects of resisting plasmodium falciparum proliferation and resisting plasmodium falciparum of different strains, and has the advantages of longer half-life period, lower plasma clearance rate, higher distribution volume and better oral bioavailability.
Synthesis method of cyclopropyl boric acid
-
Paragraph 0016; 0017; 0018; 0019, (2019/02/19)
The invention discloses a synthesis method of cyclopropyl boric acid, and belongs to the field of boric acid synthesis in organic chemistry. The synthesis method comprises the following steps: starting from formyl boric acid, enabling the formyl boric acid with strong electron-withdrawing sulfohydrazide to generate hydrazone, then introducing ethylene under the catalysis of ferriporphyrin, and reacting, thus obtaining the cyclopropyl boric acid. The synthesis method disclosed by the invention is simple in operation, the use of cyclopropyl bromide in a traditional technological method is avoided by adopting cyclopropanation reaction under metal catalysis, and a new synthesis path is provided for synthesis of the cyclopropyl boric acid.
A process for the preparation method of the cyclopropyl-boronic acid
-
Paragraph 0026; 0027; 0033; 0034; 0040; 0041, (2017/06/30)
The invention discloses a method for preparing cyclopropyl boronic acid. Cyclopropyl methanoic acid is adopted as a raw material and added into a solution obtained after n-butyllithium reacts with organic alkali at the low temperature, and then a boronizing reagent is added into the mixture; after boronation is finished, acid is added for quenching to obtain 1-carboxyl cyclopropyl boronic acid; the intermediate is added into high-boiling-point solvent and heated until the temperature is 80 DEG C-150 DEG C, after reaction deacidification, methylbenzene is added into the mixed solution for dehydration to form cyclopropyl boronic acid trimer, and the cyclopropyl boronic acid trimer is hydrolyzed to obtain the cyclopropyl boronic acid; the melting point of the obtained cyclopropyl boronic acid is 90 DEG C-95 DEG C, and the HNMR purity of the obtained cyclopropyl boronic acid is over 98%. The method is easy to operate and suitable for industrial scale-up production, and no highly toxic chemical is used in the whole process.